In vitrocytotoxicity and bioavailability of solid lipid nanoparticles containing tamoxifen citrate

Abstract

The objective of this study was to evaluate the influence of solid lipid nanoparticles (SLN) loaded with the poorly water-soluble drug tamoxifen citrate (TC) on the in vitro antitumor activity and bioavailability of the drug. TC-loaded SLN were prepared by solvent injection method using glycerol monostearate (GMS) or stearic acid (SA) as lipid matrix. Poloxamer 188 or tween 80 were used as stabilizers. TC-loaded SLN (F3 and F4) prepared using GMS and stabilized by poloxamer 188 showed highest entrapment efficiency % (86.07 ± 1.74 and 90.40 ± 1.22%) and reasonable mean particle sizes (130.40 ± 9.45 and 243.80 ± 12.33 nm), respectively. The in vitro release of TC from F3 and F4 exhibited an initial burst effect followed by a sustained drug release. In vitro cytotoxicity of F3 against human breast cancer cell line MCF-7 showed comparable antitumor activity to free drug. Moreover, the results of bioavailability evaluation of TC-loaded SLN in rats compared to free TC indicated that 160.61% increase in the oral bioavailability of TC. The obtained results suggest that incorporation of the poorly water-soluble drug TC in SLN preserves the in vitro antitumor activity and significantly enhance oral bioavailability of TC in rats.

Solid lipid nanoparticles for delivery of Calendula officinalis extract

“…The LD 50 for SLN1 was 895 µg/mL. This value was lower than the value reported for other SLN formulations composed by SA [36,37]. SLN2 presented a LD 50 value of 68.44 µg/mL whereas LD 50 for SLN3 was 151.1 µg/mL.…”

Nanostructured Lipid Carriers: Versatile Oral Delivery Vehicle

“…Numerous in vivo reports have been published till now depicting applicability of lipid nanoparticles in oral delivery; however, very few reports demonstrate the safety profile of these systems [103–105]. Reported literature reveals that biodegradable and physiological lipids used in the formulation of NLCs are well tolerated in vitro and in vivo and minimizes toxicity issues related to polymeric nanoparticles.…”

Tamoxifen-loaded solid lipid nanoparticles-induced apoptosis in breast cancer cell lines

“…[5] The antiestrogen molecule tamoxifen (TAM) is a strong, hydrophobic endocrine drug widely used for treating breast cancers and high risk patients. [6,7] Depending on the dose and the tissues targeted, the function of TAM can be estrogenic or antiestrogenic. The dosedependent side effects of TAM include liver cancer, increased blood clotting and ocular adverse effects, such as retinopathy and corneal opacities.…”